U-69593

目录号: HY-12363 纯度: 99.73%: Data Sheet SDS COA 产品使用指南
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U-69593 是一种有效且选择性的 κ1阿片受体 激动剂。U-69593 减弱成瘾剂诱导的大鼠行为敏化作用。U-69593 可减轻小鼠的焦虑并增强自发交替记忆。U-69593 降低腹侧纹状体中多巴胺和谷氨酸的钙依赖性透析液水平^[4]。

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U-69593 Chemical Structure

CAS No. : 96744-75-1

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规格	价格	是否有货
1 mg	￥1280	In-stock
5 mg	￥3200	In-stock
10 mg		询价
50 mg		询价

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

生物活性
纯度 & 产品资料
参考文献

生物活性

U-69593 is a potent and selective κ1-opioid receptor agonist^[1]. U-69593 attenuates addictive agent-induced behavioral sensitization in the rat^[2]. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice^[3]. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum^[4].

IC₅₀ & Target

κ Opioid Receptor/KOR

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.63 nM Compound: U-69593	Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593 Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593	[PMID: 9873480]
CHO	EC₅₀	0.8 nM Compound: U69,593	Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assay	[PMID: 25426797]
CHO	EC₅₀	12.5 nM Compound: U-69593	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells assessed as calcium mobilization after 1 hrs by fluorescence analysis	[PMID: 22464684]
CHO	EC₅₀	207 nM Compound: U-69593	Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding	[PMID: 16441078]
CHO	EC₅₀	207 nM Compound: U-69593	Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay Antagonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	[PMID: 17580847]
CHO	EC₅₀	26.1 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay	[PMID: 23134120]
CHO	EC₅₀	28.1 nM Compound: U-69,593	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells after 2 hrs by [35S]-GTPgammaS binding assay	[PMID: 23200250]
CHO	EC₅₀	28.1 nM Compound: U-69593	Agonist activity at human KOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay Agonist activity at human KOR expressed in CHO cell membranes by [35S]GTPgammaS binding assay	[PMID: 26346669]
CHO	EC₅₀	28.1 nM Compound: U-69,593	Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 25283554]
CHO	EC₅₀	6.6 nM Compound: U-69593	Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay Agonist activity at human kappa opioid receptor-Galpha-16 fusion protein expressed in CHO cells by calcium flux assay	[PMID: 16441078]
CHO	EC₅₀	60.14 nM Compound: U69593	Agonist activity at human kappa opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis Agonist activity at human kappa opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis	[PMID: 24657054]
CHO	EC₅₀	7.7 nM Compound: U69593	Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at rat kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 25221662]
CHO	EC₅₀	8.03 nM Compound: U-69,593	Agonist activity at human KOR expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human KOR expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 25248680]
HEK293	EC₅₀	12 nM Compound: U-69593	Agonist activity at human kappa opioid receptor expressed in HEK-293 cells assessed as stimulation of [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting analysis Agonist activity at human kappa opioid receptor expressed in HEK-293 cells assessed as stimulation of [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting analysis	[PMID: 25062506]
HEK293	EC₅₀	12 nM Compound: U-69593	Agonist activity at human kappa opioid receptor expressed in HEK-293 cells after 45 mins by [35S]GTP-gamma-S binding assay in presence of 10 uM of GDP Agonist activity at human kappa opioid receptor expressed in HEK-293 cells after 45 mins by [35S]GTP-gamma-S binding assay in presence of 10 uM of GDP	10.1039/C5MD00414D
HEK293	ED₅₀	24 nM Compound: U-69593	Effective dose for agonistic activity towards human kappa opioid receptor from membranes of HEK293 cells was determined by radiolabeled [35S]GTP-gamma-S, assay Effective dose for agonistic activity towards human kappa opioid receptor from membranes of HEK293 cells was determined by radiolabeled [35S]GTP-gamma-S, assay	[PMID: 12643930]
HEK293	EC₅₀	5.3 nM Compound: U-69,593	Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay	[PMID: 28218838]
HEK293	EC₅₀	534 nM Compound: U69593	Agonist activity at GFP-fused kappa opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay Agonist activity at GFP-fused kappa opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay	[PMID: 24613457]
HEK293	EC₅₀	80 nM Compound: U-69593	Agonist activity at human recombinant kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 45 mins by microplate luminescence assay Agonist activity at human recombinant kappa opioid receptor expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding after 45 mins by microplate luminescence assay	[PMID: 20441176]
HEK293	EC₅₀	80 nM Compound: U-69593	Agonist activity at recombinant kappa-opioid receptor in human HEK293 cells by [35S]-GTP-gammaS binding assay Agonist activity at recombinant kappa-opioid receptor in human HEK293 cells by [35S]-GTP-gammaS binding assay	[PMID: 24856182]
U2OS	EC₅₀	131 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay	[PMID: 29939744]
U2OS	EC₅₀	205 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 20 mins by Hoechst staining-based assay Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with GFP and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 20 mins by Hoechst staining-based assay	[PMID: 29939744]
U2OS	EC₅₀	5.4 nM Compound: U69,593	Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western blot analysis Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western blot analysis	[PMID: 29939744]

体内研究
(In Vivo)

U-69593 (0.16 mg/kg；sc) 减轻成瘾剂诱导的大鼠行为敏化^[2]。
U-69593 (1、10、25 nmol/μL；显微注射) 减少小鼠的焦虑并增强自发交替记忆^[3]。
U-69593 (0.32 mg/kg；sc) 降低急性苯丙胺诱发的行为和钙依赖性透析液中多巴胺和腹侧纹状体中的谷氨酸^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Rat^[2]
Dosage:	0.16 mg/kg
Administration:	S.c. (an acute injection of cocaine (20 mg/kg i.p.))
Result:	Attenuated the acute and chronic effects of cocaine on locomotor activity and stereotypy.

Animal Model:	CD-1 mice^[3]
Dosage:	1, 10, 25 nmol/µL
Administration:	Microinjection (in the infralimbic cortex (IL)), once every week, 2 weeks
Result:	Dose-dependently prolonged transfer-latency (T-L) and produced a dose-dependent anxiolytic behavioural profile, and after 24 h, the mouse were observed small but detectable carry-over effects. In week 2, U-69593 dose-dependently prolonged T/L and produced an anxiolytic behavioural profile in the first EPM (elevated plus-maze) trial, but observed a robust anxiolytic behavioural profile.

Animal Model:	280-350 g, male Wistar rats^[4]
Dosage:	0.32 mg/kg
Administration:	S.c. (followed 15 min later by an injection of amphetamine (2.5 mg/kg i.p.))
Result:	Significantly reduced the amphetamine-stimulated increase in dialysate dopamine levels and blocked the ability of amphetamine to evoke an increase in dialysate glutamate levels.

分子量

356.50

Formula

C₂₂H₃₂N₂O₂

CAS 号

96744-75-1

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (140.25 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

DMF 中的溶解度 : 10 mg/mL (28.05 mM; 超声加热助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8050 mL	14.0252 mL	28.0505 mL
5 mM	0.5610 mL	2.8050 mL	5.6101 mL
10 mM	0.2805 mL	1.4025 mL	2.8050 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.01 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.01 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.73%

选择批次：

Data Sheet (636 KB) SDS (251 KB)

COA (287 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lahti RA, et al. [3H]U-69593 a highly selective ligand for the opioid kappa receptor. Eur J Pharmacol. 1985 Feb 26;109(2):281-4. [Content Brief]

[2]. [2]Heidbreder CA, et al. The kappa-opioid receptor agonist U-69593 attenuates cocaine-induced behavioral sensitization in the rat. Brain Res. 1993 Jul 9;616(1-2):335-8. [Content Brief]

[3]. [3]Wall PM, et al. U-69,593 microinjection in the infralimbic cortex reduces anxiety and enhances spontaneous alternation memory in mice. Brain Res. 2000 Feb 21;856(1-2):259-80. [Content Brief]

[4]. [4]Gray AM, et al. The kappa-opioid agonist, U-69593, decreases acute amphetamine-evoked behaviors and calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum. J Neurochem. 1999 Sep;73(3):1066-74. [Content Brief]

U-69593 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMF / DMSO	1 mM	2.8050 mL	14.0252 mL	28.0505 mL	70.1262 mL
	5 mM	0.5610 mL	2.8050 mL	5.6101 mL	14.0252 mL
	10 mM	0.2805 mL	1.4025 mL	2.8050 mL	7.0126 mL
	15 mM	0.1870 mL	0.9350 mL	1.8700 mL	4.6751 mL
	20 mM	0.1403 mL	0.7013 mL	1.4025 mL	3.5063 mL
	25 mM	0.1122 mL	0.5610 mL	1.1220 mL	2.8050 mL
DMSO	30 mM	0.0935 mL	0.4675 mL	0.9350 mL	2.3375 mL
	40 mM	0.0701 mL	0.3506 mL	0.7013 mL	1.7532 mL
	50 mM	0.0561 mL	0.2805 mL	0.5610 mL	1.4025 mL
	60 mM	0.0468 mL	0.2338 mL	0.4675 mL	1.1688 mL
	80 mM	0.0351 mL	0.1753 mL	0.3506 mL	0.8766 mL
	100 mM	0.0281 mL	0.1403 mL	0.2805 mL	0.7013 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

U-6959396744-75-1U69593U 69593Opioid ReceptorSelectiveinfralimbic cortexanxietyspontaneous alternation memorydopamineglutamateInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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U-69593

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